Home Angiogenesis HIF inhibitor - Apoptosis related activator PX-478 2HCl For research use only.

PX-478 2HCl

PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1.

PX-478 2HCl Chemical Structure

PX-478 2HCl Chemical Structure

CAS: 685898-44-6

Selleck's PX-478 2HCl has been cited by 72 publications

Purity & Quality Control

Batch: Purity: >97%
97

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
TW03-EBV cells Function assay 10 μM 24 h suppress HIF-1α expression 30479336
H460 Function assay 10 μM reduced glucose uptake and lactate production rate 30128035
A549 Function assay 10 μM reduced glucose uptake and lactate production rate 30128035
SMMC7721 Function assay 25 μM 24 h inhibits migration of SMMC7721 29495380
EC9706 Function assay 20 μM PX-478 inhibited normoxic and hypoxia-induced HIF-1α expression as well as COX-2 and PD-L1 expression 28560067
EC109 Function assay 20 μM PX-478 inhibited normoxic and hypoxia-induced HIF-1α expression as well as COX-2 and PD-L1 expression 28560067
Tca8113 Function assay 0, 5, and 25 μM 24 h reduces cellular autophagy 26640316
PDAC cell lines Function assay 25 μM 24 h induced a translocation of HMGB1 from the nucleus to the cytoplasm 25544770
PC3 Function assay 20 hr IC50 for HIF-1α inhibition for PC3 cells under normoxic condition was 20-25 μmol/L 18729192
DU 145 Function assay 20 hr IC50 for HIF-1α inhibition for the DU 145 cells was ~40-50 μmol/L 18729192
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs under hypoxic condition by MTT assay, IC50 = 19.7 μM. 28209257
MCF7 Function assay 24 hrs Inhibition of HIF-1alpha (unknown origin) transcriptional activity expressed in human MCF7 cells after 24 hrs under hypoxic condition by HRE luciferase reporter gene assay , IC50 = 20.2 μM. 28209257
MDA-MB-468 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-468 cells after 72 hrs under hypoxic condition by MTT assay, IC50 = 45.1 μM. 28209257
Click to View More Cell Line Experimental Data

Biological Activity

Description PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1.
Targets
HIF-1α [1]
In vitro
In vitro

PX-478 lowers HIF-1α protein levels and HIF-1 transactivation in hypoxia and in normoxia in a variety of cancer cell lines, but has a more pronounced effect on translation of proteins, such as HIF-1α in hypoxia. [2]

PX-478 also enhances the radiosensitivity of prostate carcinoma PC3 cells. [3]
Cell Research Cell lines NPC cell lines
Concentrations 10 μM
Incubation Time 24 h
Method

Cells were treated with 10 or 50 μM PX-478
Experimental Result Images Methods Biomarkers Images PMID
Western blot HIF-1α VEGF / Angiopoietin 1 E-cadherin / N-cadherin / Vimentin HIF-1α VEGF / Angiopoietin 1 E-cadherin / N-cadherin / Vimentin 18729192
Growth inhibition assay Cell viability Cell viability 28052321
In Vivo
In vivo

In HT-29 human colon cancer xenografts, PX-478 suppresses HIF-1alpha levels and inhibits the expression of HIF-1 target genes including vascular endothelial growth factor and the glucose transporter-1. In addition, PX-478 (100 or 120 mg/kg i.p.) also shows antitumor activity including cures against several established human tumor xenografts that is related to the levels of HIF-1α. [1]

In high-fat-diet mice, PX-478 causes reduced fibrosis and fewer inflammatory infiltrates in their adipose tissues. [4]
Animal Research Animal Models Mice bearing MCF-7 human breast cancer, HT-29 colon cancer, PC-3 prostate cancer, DU-145 prostate cancer, OvCar-3 ovarian cancer, A-549 non-small cell lung cancer, SHP-77 small cell lung cancer, and Caki-1 renal cancer, Panc-1, MiaPaCa, or BxPC-3 pancreatic cancer xenografts.
Dosages 100 or 120 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00522652 Completed Advanced Solid Tumors|Lymphoma Cascadian Therapeutics Inc.|Seagen Inc. August 2007 Phase 1

Chemical lnformation & Solubility

Molecular Weight 394.12 Formula

C13H20Cl4N2O3
CAS No. 685898-44-6 SDF Download PX-478 2HCl SDF
Smiles C1=CC(=CC=C1CC(C(=O)O)N)[N+](CCCl)(CCCl)[O-].Cl.Cl
Storage (From the date of receipt) 3 years -20°C powder (seal)

In vitro
Batch:

DMSO : 79 mg/mL ( (200.44 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 79 mg/mL

Ethanol : 79 mg/mL


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In vivo
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